Screening of solubilization potential of various green excipients for case of hydrophobic antituberculous thioacetazone

The present study is aimed at solving the problem of poor solubility of the antituberculosis drug thioacetazone (TAZ), the use of which, despite its effectiveness, is limited by toxicity and requires a reduction of the therapeutic dose. Such representatives of "green chemistry" as a deep eutectic solvent based on choline chloride with urea, native and modified cyclodextrins (I3-CD and HP-I3-CD) and biocompatible polymers (PVP and PEG) were used as solubilizing agents. DES and modified HP-I3-CD proved to be the most effective, improving water solubility of TAZ by 106 and 24 times, respectively. I3-CD and polymers showed a weak solubilizing potential, demonstrating the ineffectiveness of their application to reduce the hydrophobicity of the drug. In addition, the effect of temperature and concentration of excipients in an aqueous medium on drug dissolution was studied. The thermodynamic aspects of the dissolution and complex formation processes of in the selected systems are also characterized.